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Vol. 59, Issue 3, 420-426, March 2001
The R. W. Johnson Pharmaceutical Research Institute, San
Diego, California
Histamine is a multifunctional hormone that regulates smooth muscle
contraction in the airways, acid secretion in the gut, and
neurotransmitter release in the central nervous system through three
well characterized receptor subtypes, H1, H2,
H3, respectively. As part of a directed effort to discover
novel G-protein-coupled receptors through homology searching of genomic
databases, we identified a partial clone (GPCR105) that had significant
homology to the recently identified histamine H3 receptor
cDNA. Expression of the full-length human GPCR105 in cells confers the
ability to bind [3H]histamine with high affinity
(KD = 5 nM). GPCR105 is
pharmacologically similar to the histamine H3 receptor in
that it binds many of the known H3 agonists and
antagonists, albeit with a different rank order of affinity/potency.
GPCR105 does not bind (i.e., KD > 10 µM) all tested H1 and H2 receptor antagonists
such as diphenhydramine, loratadine, ranitidine, and cimetidine, but
has modest affinity for the H2 receptor agonist, dimaprit
(377 nM). Whereas the H3 receptor is expressed almost
exclusively in nervous tissues, GPRC105 is expressed primarily in bone
marrow and eosinophils. Together, these data demonstrate that GPCR105
is a novel histamine receptor structurally and pharmacologically
related to the H3 receptor. However, its unique expression
profile and physiological role suggest that GPCR105 is a fourth
histamine receptor subtype (H4) and may be a therapeutic
target for the regulation of immune function, particularly with respect
to allergy and asthma.
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